Sulphapyridine composition of low toxicity



' Patented May 22, 1945 Gustav J. Martin, Elmhurst, and Marvin R. Thompson, Great Neck,- N. Y., assignors to William R. Warner .& Company, Inc., New York, N. Y., a corporation of Delaware No Drawing. Application May 11, 1940,

Serial No. 334,653

2 Claims. (01. 7-65) This invention relates to therapeutic materials of lowered toxicity. More particularly, it relates to therapeutic agents comprising sulphapyridine f in association with material lowering the toxicity thereof.

Sulphapyridine is a drug that is widely used in the treatment of diseases or infections caused by certain micro-organisms, notably pneumonia and aflect its therapeutic eiiect cannot be predicted from any available knowledge.

We have discovered that ii glycine or an equivalent compound, is administered at the same time as the sulphapyridine, the toxic properties of sul-' phapyridine on the human system are eliminatsimilar diseases, The sulphapyridine is generally regarded as achieving its therapeutic effect by destroying or aflecting the micro-organism. The amount of the drug that may be administered in the treatment of the disease, however, is usually less than the amount that would obtain the maxv imum, or in many cases a suiiicient or desirable, therapeutic eiiect. This limit is occasioned by the toxic action of the sulphapyridine. This is one of the principal diillculties involved in the administration of sulphapyridine. In many cases.

where the disease is advanced, the patient cannot tolerate a sumcient amount of the drug to check the action of the micro-organisms. In other cases-the tolerance of the patient is so low as to make it impossible to use an eflective amount of the sulphapyridine and it therefore cannot be used as a therapeutic measure.

' It is an object of our invention to provide a therapeutic agent, comprising sulphapyridine which is non-toxic or 0! reduced toxicity and which can be administered in greater amounts in most cases, or at least in the usual amounts without an objectionable toxic eflect on the human being.

As is apparent iromthe above description, the

' sulphapyridine has two characteristics; one is its therapeutic efiect achieved through its actionon the micro-organisms and the other is its toxic e1- iect resulting from the toxic action of the sulphapyridine on the animal body, It would be relatively simple to modify the sulphapyridine or its action so as to alter its toxicity along with its therapeutic eflect. However, it is not a simple matter to alter one of these characteristics without altering the other, i. e., to alter the toxicity without destroying the therapeutic eflect.

The action and theory oi detoxication has been appreciated heretofore, and in general; a detoxitying material is thought to combine or coact with the drug in the body in such a manner as to mask the toxic characteristic while leaving unaltered the structural characteristic of the compound that is responsible i'or the therapeutic eiiect. But the exact action of various materials is little known, and the nature 0! detoxicants or theiractionwithapartieulardrugeoasnotto ed or greatly reduced and minimized, but at the 7 same time the therapeutic eflect oi the sulphapyridine is not appreciably interfered with. It

is possible, therefore, to give a dosage oi the suiphapyridine which is eilective in its action against the micro-organisms without adversely ailecting the patient. a

It is a iurther object or our invention therefore to provide a therapeutic agent comprising in combination sulphapyridine with glycine and its equivalents, i. e., its precursors and biochemically related compounds. I

In accordance with our invention, the sulphapyridine may be admixed in the desired proportions with the glycine or equivalent compounds in either a dry mixture or in solution. This mixture may then be administered in the same way that sulphapyridine' is normally administered, namely, orally, parenterally, rectally, etc. While the glycine acid may be administered to the human body separately from the sulphapyridine, we find it more convenient to administer them as a mixture since this assures that the proper amount of both ingredients will be at the same time, and also eliminates the necessity for administering two drugs which would be less convenient and might give rise to misunderstanding as to the amount and nature of the administration,

Upon being taken into the body, the sulphapyridine and glycine coact or react to produce a material having the non-toxic, therapeutic eflect. Ii desired, the, sulphapyridine and glycine may be reacted in the laboratory in a manner similar to the action that takes place in the body in order to provide a single new compound which may be administered to produce the non-toxic therapeutic eflect. Such compounds are hitherto unknown.

The proportions of the materials are not criti-' cal, since glycine is i'ound in and formed from dietary components and may therefore be viewed as foods for the human body. They may betakeninto the body in relatively large amounts without any harmful action. The upper limit 01' the proportion of glycine in our composition ing -1 to 50 parts of glycine in admixture with 6 parts of sulphapyridine to be suitable in most inf 1 therapeutic eil'ect thereof.

stances. Satisfactory results are usually obtained when the mixture comprises equal parts. 3 It will be apparent that we have provided 1 therapeutic material having superior and advan- 3 tageous non-toxic properties, as described in the specification and following claims forming a part thereof.

We claim:

1. A therapeutic agentior use in connection with the treatment oi diseases caused by microorganisms, comprising sulphapyridine for combattlng said micro-organisms and disease, in as.- sociation with glycine to lower the toxicity of said sulphapyridlne without materially impairing the 2. A therapeutic composition of matter consisting of sulphapyridine and llycine.

' GUSTAV J. MARTIN.

MARVIH R. THOMPSON. 

